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Bioorg Med Chem Lett. 2009 May 1;19(9):2482-6. doi: 10.1016/j.bmcl.2009.03.057. Epub 2009 Mar 18.

Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety.

Author information

1
Department of Chemical Research-CV & CNS, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.

Abstract

A series of nortropane analogs based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high affinity. The synthesis and structure-activity relationships around the C-3 nortropane substitution are described. From the SAR study and hPXR screening effort, compound 15 was identified to possess potent oral antitussive and anxiolytic-like activities in the guinea pig models.

PMID:
19332374
DOI:
10.1016/j.bmcl.2009.03.057
[Indexed for MEDLINE]

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